JP5705580B2 - チオアミド化合物、チオアミド化合物の製造方法、［（４ｒ，６ｒ）−６−アミノエチル−１，３−ジオキサン−４−イル］アセテート誘導体の製造方法、及びアトルバスタチンの製造方法 - Google Patents

チオアミド化合物、チオアミド化合物の製造方法、［（４ｒ，６ｒ）−６−アミノエチル−１，３−ジオキサン−４−イル］アセテート誘導体の製造方法、及びアトルバスタチンの製造方法 Download PDF

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JP5705580B2
JP5705580B2 JP2011035006A JP2011035006A JP5705580B2 JP 5705580 B2 JP5705580 B2 JP 5705580B2 JP 2011035006 A JP2011035006 A JP 2011035006A JP 2011035006 A JP2011035006 A JP 2011035006A JP 5705580 B2 JP5705580 B2 JP 5705580B2
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general formula
compound represented
group
converting
hydrogen atom
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JP2012171904A (ja
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柴崎　正勝
正勝 柴崎
直哉 熊谷
直哉 熊谷
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Microbial Chemistry Research Foundation
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Microbial Chemistry Research Foundation
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Priority to EP12750077.5A priority patent/EP2679580B1/en
Priority to PCT/JP2012/053323 priority patent/WO2012114926A1/ja
Priority to CN201280009635.7A priority patent/CN103384659B/zh
Publication of JP2012171904A publication Critical patent/JP2012171904A/ja
Priority to IL228027A priority patent/IL228027A/en
Priority to US13/971,186 priority patent/US8785690B2/en
Priority to HK14100943.2A priority patent/HK1187892A1/xx
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C327/00—Thiocarboxylic acids
    • C07C327/38—Amides of thiocarboxylic acids
    • C07C327/40—Amides of thiocarboxylic acids having carbon atoms of thiocarboxamide groups bound to hydrogen atoms or to acyclic carbon atoms
    • C07C327/42—Amides of thiocarboxylic acids having carbon atoms of thiocarboxamide groups bound to hydrogen atoms or to acyclic carbon atoms to hydrogen atoms or to carbon atoms of a saturated carbon skeleton
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/08—Drugs for disorders of the urinary system of the prostate
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/06—Antihyperlipidemics
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B53/00—Asymmetric syntheses
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/30—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members
    • C07D207/32—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • C07D207/33—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms with substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • C07D207/337—Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/30—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members
    • C07D207/34—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F7/00—Compounds containing elements of Groups 4 or 14 of the Periodic Table
    • C07F7/02—Silicon compounds
    • C07F7/08—Compounds having one or more C—Si linkages
    • C07F7/18—Compounds having one or more C—Si linkages as well as one or more C—O—Si linkages
    • C07F7/1804—Compounds having Si-O-C linkages
    • Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02P—CLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
    • Y02P20/00—Technologies relating to chemical industry
    • Y02P20/50—Improvements relating to the production of bulk chemicals
    • Y02P20/55—Design of synthesis routes, e.g. reducing the use of auxiliary or protecting groups

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Neurosurgery (AREA)
  • Rheumatology (AREA)
  • Biomedical Technology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Neurology (AREA)
  • Obesity (AREA)
  • Psychiatry (AREA)
  • Hospice & Palliative Care (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Urology & Nephrology (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
  • Pyrrole Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
JP2011035006A 2011-02-21 2011-02-21 チオアミド化合物、チオアミド化合物の製造方法、［（４ｒ，６ｒ）−６−アミノエチル−１，３−ジオキサン−４−イル］アセテート誘導体の製造方法、及びアトルバスタチンの製造方法 Expired - Fee Related JP5705580B2 (ja)

Priority Applications (7)

Application Number Priority Date Filing Date Title
JP2011035006A JP5705580B2 (ja) 2011-02-21 2011-02-21 チオアミド化合物、チオアミド化合物の製造方法、［（４ｒ，６ｒ）−６−アミノエチル−１，３−ジオキサン−４−イル］アセテート誘導体の製造方法、及びアトルバスタチンの製造方法
PCT/JP2012/053323 WO2012114926A1 (ja) 2011-02-21 2012-02-14 チオアミド化合物、チオアミド化合物の製造方法、［（４ｒ，６ｒ）－６－アミノエチル－１，３－ジオキサン－４－イル］アセテート誘導体の製造方法、及びアトルバスタチンの製造方法
CN201280009635.7A CN103384659B (zh) 2011-02-21 2012-02-14 硫代酰胺化合物及生产该化合物、[(4r,6r)-6-氨乙基-1,3-二噁烷-4-基]乙酸酯衍生物和阿托伐他汀的方法
EP12750077.5A EP2679580B1 (en) 2011-02-21 2012-02-14 Thioamide compound, method for producing thioamide compound, method for producing [(4r,6r)-6-aminoethyl-1,3-dioxan-4-yl]acetate derivative, and method for producing atorvastatin
IL228027A IL228027A (en) 2011-02-21 2013-08-19 Composition of theomide, a method for the production of theomide, a method of producing a derivative of - 3, 1 - aminoethyl - 6 (r6, r4)] acetate [yl - 4 - dioxane, and a method of producing atorvastatin
US13/971,186 US8785690B2 (en) 2011-02-21 2013-08-20 Thioamide compound, method for producing thioamide compound, method for producing [(4R,6R)-6-aminoethyl-1,3-dioxan-4-yl]acetate derivative, and method for producing atorvastatin
HK14100943.2A HK1187892A1 (en) 2011-02-21 2014-01-29 Thioamide compound, and method for producing the compound,[(4r,6r)-6- aminoethyl-1,3-dioxane-4-yl]acetate derivative and atorvastatin [(4r6r)-6--13--4-]

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JP2011035006A JP5705580B2 (ja) 2011-02-21 2011-02-21 チオアミド化合物、チオアミド化合物の製造方法、［（４ｒ，６ｒ）−６−アミノエチル−１，３−ジオキサン−４−イル］アセテート誘導体の製造方法、及びアトルバスタチンの製造方法

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JP2012171904A JP2012171904A (ja) 2012-09-10
JP5705580B2 true JP5705580B2 (ja) 2015-04-22

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JP2011035006A Expired - Fee Related JP5705580B2 (ja) 2011-02-21 2011-02-21 チオアミド化合物、チオアミド化合物の製造方法、［（４ｒ，６ｒ）−６−アミノエチル−１，３−ジオキサン−４−イル］アセテート誘導体の製造方法、及びアトルバスタチンの製造方法

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US (1) US8785690B2 (xx)
EP (1) EP2679580B1 (xx)
JP (1) JP5705580B2 (xx)
CN (1) CN103384659B (xx)
HK (1) HK1187892A1 (xx)
IL (1) IL228027A (xx)
WO (1) WO2012114926A1 (xx)

Families Citing this family (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP5986872B2 (ja) * 2012-10-05 2016-09-06 公益財団法人微生物化学研究会 化合物、該化合物の製造方法、アセテート誘導体の製造方法、及びアトルバスタチンの製造方法、並びに不斉配位子の回収方法
CN105503815A (zh) * 2014-09-22 2016-04-20 兰州大学 一种立普妥合成中间体的制备方法

Family Cites Families (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
FI94339C (fi) 1989-07-21 1995-08-25 Warner Lambert Co Menetelmä farmaseuttisesti käyttökelpoisen /R-(R*,R*)/-2-(4-fluorifenyyli)- , -dihydroksi-5-(1-metyylietyyli)-3-fenyyli-4-/(fenyyliamino)karbonyyli/-1H-pyrroli-1-heptaanihapon ja sen farmaseuttisesti hyväksyttävien suolojen valmistamiseksi
CN1127503C (zh) * 2000-12-08 2003-11-12 中国科学院上海有机化学研究所 （r）－2－[3－（2－n－邻苯二甲酰亚胺基乙基）－4，5－二氢－5－异噁唑基]－乙酸、合成及用途
CZ292221B6 (cs) * 2001-06-29 2003-08-13 Léčiva, A. S. Způsob výroby (4R,6R) terc-butyl[6-(2-aminoethyl)-2,2-dimethyl[1,3]dioxan-4-yl]acetátu a meziproduktů pro jeho výrobu
JP4578240B2 (ja) 2002-08-09 2010-11-10 コデクシス， インコーポレイテッド ４−置換３−ヒドロキシ酪酸誘導体の生成のための酵素的プロセス
GB0317393D0 (en) * 2003-07-25 2003-08-27 Avecia Ltd Process and compounds
EP1893767A1 (en) * 2005-06-16 2008-03-05 Pfizer, Inc. Process for producing atorvastatin, pharmaceutically acceptable salts thereof and intermediates thereof
ATE432276T1 (de) * 2005-09-09 2009-06-15 Pfizer Science & Tech Ltd Herstellung eines atorvastatin-zwischenprodukts
US20090216029A1 (en) * 2005-09-16 2009-08-27 Yatendra Kumar Process for the production of atorvastatin calcium in amorphous form
WO2007034909A1 (ja) * 2005-09-22 2007-03-29 Kaneka Corporation （３ｒ，５ｒ）－７－アミノ－３，５－ジヒドロキシヘプタン酸誘導体の製造法
CN101805279A (zh) * 2010-01-22 2010-08-18 绍兴民生医药有限公司 阿托伐他汀钙的制备方法

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Publication number Publication date
EP2679580A4 (en) 2015-09-09
US8785690B2 (en) 2014-07-22
JP2012171904A (ja) 2012-09-10
EP2679580A1 (en) 2014-01-01
CN103384659A (zh) 2013-11-06
CN103384659B (zh) 2015-11-25
HK1187892A1 (en) 2014-04-17
EP2679580B1 (en) 2017-08-09
WO2012114926A1 (ja) 2012-08-30
US20130338375A1 (en) 2013-12-19
IL228027A0 (en) 2013-09-30
IL228027A (en) 2015-05-31

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